CN101006097B - Vla-4拮抗剂 - Google Patents

Vla-4拮抗剂 Download PDF

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Publication number
CN101006097B
CN101006097B CN2005800277189A CN200580027718A CN101006097B CN 101006097 B CN101006097 B CN 101006097B CN 2005800277189 A CN2005800277189 A CN 2005800277189A CN 200580027718 A CN200580027718 A CN 200580027718A CN 101006097 B CN101006097 B CN 101006097B
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China
Prior art keywords
compound
acid
formula
alkylsulfonyl
amino
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Expired - Fee Related
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CN2005800277189A
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English (en)
Chinese (zh)
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CN101006097A (zh
Inventor
陈为桥
A·D·莱布萨克
B·穆诺斯
S·文卡特拉曼
王波维
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Merck Sharp and Dohme LLC
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Schering Corp
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05—Dipeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
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    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pulmonology (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
CN2005800277189A 2004-08-16 2005-08-12 Vla-4拮抗剂 Expired - Fee Related CN101006097B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US60194204P 2004-08-16 2004-08-16
US60/601,942 2004-08-16
PCT/US2005/028768 WO2006023396A2 (en) 2004-08-16 2005-08-12 Vla-4 antagonists

Publications (2)

Publication Number Publication Date
CN101006097A CN101006097A (zh) 2007-07-25
CN101006097B true CN101006097B (zh) 2012-07-11

Family

ID=35502447

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2005800277189A Expired - Fee Related CN101006097B (zh) 2004-08-16 2005-08-12 Vla-4拮抗剂

Country Status (15)

Country Link
US (1) US7776891B2 (de)
EP (1) EP1781686B1 (de)
JP (1) JP4649476B2 (de)
KR (1) KR20070044054A (de)
CN (1) CN101006097B (de)
AT (1) ATE430761T1 (de)
AU (1) AU2005277634B2 (de)
BR (1) BRPI0514415A (de)
CA (1) CA2576647C (de)
DE (1) DE602005014364D1 (de)
IL (1) IL181267A0 (de)
MX (1) MX2007001876A (de)
NO (1) NO20071399L (de)
RU (1) RU2007109601A (de)
WO (1) WO2006023396A2 (de)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2604531A1 (en) * 2005-04-21 2006-11-02 Merck And Co., Inc. Vla-4 antagonists
AU2008266960A1 (en) 2007-06-20 2008-12-24 Merck Sharp & Dohme Corp. Diphenyl substituted alkanes
US10836720B2 (en) 2016-04-01 2020-11-17 The Regents Of The University Of California Inhibitors of integrin alpha 5 beta 1 and methods of use
CA3114240C (en) 2018-10-30 2023-09-05 Gilead Sciences, Inc. Imidazopyridine derivatives as alpha4beta7 integrin inhibitors
CA3115830C (en) 2018-10-30 2023-09-12 Gilead Sciences, Inc. Compounds for inhibition of .alpha.4.beta.7 integrin
AU2019373240B2 (en) 2018-10-30 2023-04-20 Gilead Sciences, Inc. Quinoline derivatives as alpha4beta7 integrin inhibitors
US11224600B2 (en) 2018-10-30 2022-01-18 Gilead Sciences, Inc. Compounds for inhibition of alpha 4 beta 7 integrin
WO2021030438A1 (en) 2019-08-14 2021-02-18 Gilead Sciences, Inc. Compounds for inhibition of alpha 4 beta 7 integrin

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002074761A1 (en) * 2001-03-20 2002-09-26 Merck & Co., Inc. Substituted n-arylsulfonyl-proline derivatives as potent cell adhesion inhibitors
CN1391473A (zh) * 1999-06-30 2003-01-15 第一制药株式会社 Vla－4抑制剂化合物
CN1402709A (zh) * 1999-12-06 2003-03-12 霍夫曼-拉罗奇有限公司 4－吡啶基－n－酰基－l－苯丙氨酸
CN1407972A (zh) * 1999-12-06 2003-04-02 霍夫曼-拉罗奇有限公司 4－嘧啶基－n－酰基－l－苯基丙氨酸类化合物

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6291511B1 (en) 1997-05-29 2001-09-18 Merck & Co., Inc. Biarylalkanoic acids as cell adhesion inhibitors
US6903075B1 (en) 1997-05-29 2005-06-07 Merck & Co., Inc. Heterocyclic amide compounds as cell adhesion inhibitors
US6583139B1 (en) * 1997-07-31 2003-06-24 Eugene D. Thorsett Compounds which inhibit leukocyte adhesion mediated by VLA-4
US6455550B1 (en) 1997-08-22 2002-09-24 Hoffmann-La Roche Inc. N-alkanoylphenylalanine derivatives
US6229011B1 (en) 1997-08-22 2001-05-08 Hoffman-La Roche Inc. N-aroylphenylalanine derivative VCAM-1 inhibitors
US6338084B1 (en) * 1998-12-17 2002-01-08 International Business Machines Corporation Method for process-specific exchange of data between machines in a network
NZ513254A (en) 1999-02-18 2003-10-31 F Thioamide derivatives
WO2001036376A1 (fr) 1999-11-18 2001-05-25 Ajinomoto Co., Inc. Nouveaux dérivés de la phénylalanine
US6388084B1 (en) 1999-12-06 2002-05-14 Hoffmann-La Roche Inc. 4-pyridinyl-n-acyl-l-phenylalanines
US6559174B2 (en) 2001-03-20 2003-05-06 Merck & Co., Inc. N-arylsulfonyl aryl aza-bicyclic derivatives as potent cell adhesion inhibitors
US6855708B2 (en) 2001-03-20 2005-02-15 Merck & Co., Inc. N-arylsulfonyl aza-bicyclic derivatives as potent cell adhesion inhibitors
TW200307671A (en) 2002-05-24 2003-12-16 Elan Pharm Inc Heteroaryl compounds which inhibit leukocyte adhesion mediated by α 4 integrins
WO2005087760A1 (en) 2004-03-10 2005-09-22 Merck & Co., Inc. Vla-4 antagonists

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1391473A (zh) * 1999-06-30 2003-01-15 第一制药株式会社 Vla－4抑制剂化合物
CN1402709A (zh) * 1999-12-06 2003-03-12 霍夫曼-拉罗奇有限公司 4－吡啶基－n－酰基－l－苯丙氨酸
CN1407972A (zh) * 1999-12-06 2003-04-02 霍夫曼-拉罗奇有限公司 4－嘧啶基－n－酰基－l－苯基丙氨酸类化合物
WO2002074761A1 (en) * 2001-03-20 2002-09-26 Merck & Co., Inc. Substituted n-arylsulfonyl-proline derivatives as potent cell adhesion inhibitors

Also Published As

Publication number Publication date
CN101006097A (zh) 2007-07-25
IL181267A0 (en) 2007-07-04
BRPI0514415A (pt) 2008-06-10
WO2006023396A3 (en) 2006-04-27
US20070219252A1 (en) 2007-09-20
AU2005277634B2 (en) 2011-02-17
NO20071399L (no) 2007-05-08
KR20070044054A (ko) 2007-04-26
CA2576647C (en) 2011-12-13
RU2007109601A (ru) 2008-09-27
JP2008510005A (ja) 2008-04-03
EP1781686A2 (de) 2007-05-09
JP4649476B2 (ja) 2011-03-09
ATE430761T1 (de) 2009-05-15
DE602005014364D1 (de) 2009-06-18
WO2006023396A2 (en) 2006-03-02
EP1781686B1 (de) 2009-05-06
MX2007001876A (es) 2007-05-09
CA2576647A1 (en) 2006-03-02
US7776891B2 (en) 2010-08-17
AU2005277634A1 (en) 2006-03-02

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